559404
SB 239063
A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the α- and β-isoforms (IC50 = 44 nM), but not the γ- or δ-isoform (IC50 > 100 µM), of MAP kinase p38.
别名:
SB 239063, trans-1-(4-Hydroxycyclohexyl)-4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazole, p38 MAP Kinase Inhibitor XV
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关于此项目
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
InChI
1S/C20H21FN4O2/c1-27-20-22-11-10-17(24-20)19-18(13-2-4-14(21)5-3-13)23-12-25(19)15-6-8-16(26)9-7-15/h2-5,10-12,15-16,26H,6-9H2,1H3
InChI key
ZQUSFAUAYSEREK-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 0.5-1 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
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General description
A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the α and β isoforms (IC50 = 44 nM), but not the γ or δ isoforms (IC50 >100 µM) of p38 MAP kinase. Inhibits IL-1 and TNF-a production in LPS-stimulated human peripheral blood monocytes (IC50 = 120 nM and 350 nM, respectively). Reported to protect against mild excitotoxic neuronal injury caused by NMDA and provides substantial protection against cell death induced by either oxygen glucose deprivation (OGD) or magnesium deprivation in cultured neurons. Also reported to reduce myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of polymorphonuclear (PMN) accumulation.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MAPKp38α & β
MAPKp38α & β
Product competes with ATP.
Reversible: yes
Target IC50: 44 nM against of the α- and β-isoforms of MAP kinase p38; <100 µM against the γ- or δ-isoform of MAP kinase p38
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
May require slight warming to achieve complete solubilization.
Other Notes
Gao, F., et al. 2002. Cardiovasc. Res.53, 414.
Ju, H., et al. 2002. J. Pharmacol. Exp. Ther.301, 15.
Legos, J.J., et al. 2002. Eur. J. Pharmacol.447, 37.
Barone, F.C., et al. 2001. J. Pharmacol. Exp. Ther.296, 312.
Ward, K.W., et al. 2001. Pharm. Res.18, 1336.
Underwood, D.C., et al. 2000. J. Pharmacol. Exp. Ther.293, 281.
Underwood, D.C., et al. 2000. Am. J. Physiol. Lung Cell Mol. Physiol.279, L895.
Ju, H., et al. 2002. J. Pharmacol. Exp. Ther.301, 15.
Legos, J.J., et al. 2002. Eur. J. Pharmacol.447, 37.
Barone, F.C., et al. 2001. J. Pharmacol. Exp. Ther.296, 312.
Ward, K.W., et al. 2001. Pharm. Res.18, 1336.
Underwood, D.C., et al. 2000. J. Pharmacol. Exp. Ther.293, 281.
Underwood, D.C., et al. 2000. Am. J. Physiol. Lung Cell Mol. Physiol.279, L895.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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